New chalcone and pterocarpoid derivatives from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property

  • Fitoterapia. 2016 Jul;112:222-8. doi: 10.1016/j.fitote.2016.06.003.
Wen-Jia Kang  1 ,  Da-Hong Li  1 ,  Tong Han  1 ,  Lin Sun  1 ,  Yan-Bin Fu  1 ,  Chun-Mei Sai  1 ,  Zhan-Lin Li  2 ,  Hui-Ming Hua  3
Affiliations
  • 1. Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • 2. Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: [email protected].
  • 3. Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: [email protected].
PMID: 27316977 DOI: 10.1016/j.fitote.2016.06.003
Abstract

Investigation of the roots of Flemingia philippinensis resulted in the isolation of two new Chalcones, flemiphilippinones B (1) and C (2), and one new pterocarpoid, demethylwedelolactone-11-methyl ether (3), together with 12 known compounds (4-15). The antiproliferative activity against PC-3 cells was evaluated and most compounds showed cytotoxicity, among which, compound 2 exhibited GI50 value of 14.12μM. The antiproliferative activity of 2 against Bel-7402 and CaEs-17 cells was also measured, with GI50 values of 1.91 and 2.58μM, respectively. Intensive mechanism study showed that 2 caused cell-cycle arrest at S/G2 phase and induced Apoptosis in Bel-7402 cells through mitochondria-related pathway.

Keywords
Apoptosis; Chalcone; Flemingia philippinensis; Leguminosae; Pterocarpoid.
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